DE69731544T2 - Trizyklische antitumor verbindungen mit farnesyl protein transferase inhibierender wirkung - Google Patents
Trizyklische antitumor verbindungen mit farnesyl protein transferase inhibierender wirkung Download PDFInfo
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- DE69731544T2 DE69731544T2 DE69731544T DE69731544T DE69731544T2 DE 69731544 T2 DE69731544 T2 DE 69731544T2 DE 69731544 T DE69731544 T DE 69731544T DE 69731544 T DE69731544 T DE 69731544T DE 69731544 T2 DE69731544 T2 DE 69731544T2
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- RLOWWWKZYUNIDI-UHFFFAOYSA-N phosphinic chloride Chemical compound ClP=O RLOWWWKZYUNIDI-UHFFFAOYSA-N 0.000 description 1
- 230000006461 physiological response Effects 0.000 description 1
- 125000004193 piperazinyl group Chemical group 0.000 description 1
- 150000003053 piperidines Chemical class 0.000 description 1
- 125000005936 piperidyl group Chemical group 0.000 description 1
- 239000013612 plasmid Substances 0.000 description 1
- 231100000614 poison Toxicity 0.000 description 1
- 230000007096 poisonous effect Effects 0.000 description 1
- 229920002401 polyacrylamide Polymers 0.000 description 1
- 239000000256 polyoxyethylene sorbitan monolaurate Substances 0.000 description 1
- 235000010486 polyoxyethylene sorbitan monolaurate Nutrition 0.000 description 1
- 229920000137 polyphosphoric acid Polymers 0.000 description 1
- 229910000027 potassium carbonate Inorganic materials 0.000 description 1
- WVUCPRGADMCTBN-UHFFFAOYSA-M potassium;3-ethoxy-3-oxopropanoate Chemical compound [K+].CCOC(=O)CC([O-])=O WVUCPRGADMCTBN-UHFFFAOYSA-M 0.000 description 1
- 230000036515 potency Effects 0.000 description 1
- 230000013823 prenylation Effects 0.000 description 1
- 238000012545 processing Methods 0.000 description 1
- 125000006239 protecting group Chemical group 0.000 description 1
- 239000012264 purified product Substances 0.000 description 1
- 125000004307 pyrazin-2-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 description 1
- 238000001953 recrystallisation Methods 0.000 description 1
- 206010038038 rectal cancer Diseases 0.000 description 1
- 208000020615 rectal carcinoma Diseases 0.000 description 1
- 238000007363 ring formation reaction Methods 0.000 description 1
- 239000012723 sample buffer Substances 0.000 description 1
- 230000007017 scission Effects 0.000 description 1
- 238000006748 scratching Methods 0.000 description 1
- 230000002393 scratching effect Effects 0.000 description 1
- 238000010898 silica gel chromatography Methods 0.000 description 1
- 239000002356 single layer Substances 0.000 description 1
- 235000017557 sodium bicarbonate Nutrition 0.000 description 1
- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 1
- 159000000000 sodium salts Chemical class 0.000 description 1
- 239000007909 solid dosage form Substances 0.000 description 1
- 229940124530 sulfonamide Drugs 0.000 description 1
- 150000003456 sulfonamides Chemical class 0.000 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-N sulfuric acid Substances OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- QHOKENWFMZXSEU-UHFFFAOYSA-N tetrabutylazanium;nitrate Chemical compound [O-][N+]([O-])=O.CCCC[N+](CCCC)(CCCC)CCCC QHOKENWFMZXSEU-UHFFFAOYSA-N 0.000 description 1
- BRNULMACUQOKMR-UHFFFAOYSA-N thiomorpholine Chemical compound C1CSCCN1 BRNULMACUQOKMR-UHFFFAOYSA-N 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 238000005809 transesterification reaction Methods 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
- 230000001052 transient effect Effects 0.000 description 1
- 230000010474 transient expression Effects 0.000 description 1
- YNJBWRMUSHSURL-UHFFFAOYSA-N trichloroacetic acid Chemical compound OC(=O)C(Cl)(Cl)Cl YNJBWRMUSHSURL-UHFFFAOYSA-N 0.000 description 1
- ITMCEJHCFYSIIV-UHFFFAOYSA-N triflic acid Chemical compound OS(=O)(=O)C(F)(F)F ITMCEJHCFYSIIV-UHFFFAOYSA-N 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US71298996A | 1996-09-13 | 1996-09-13 | |
| US712989 | 1996-09-13 | ||
| US87740097A | 1997-06-17 | 1997-06-17 | |
| US877400 | 1997-06-17 | ||
| PCT/US1997/015899 WO1998011092A1 (en) | 1996-09-13 | 1997-09-11 | Tricyclic antitumor compounds being farnesyl protein transferase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| DE69731544D1 DE69731544D1 (de) | 2004-12-16 |
| DE69731544T2 true DE69731544T2 (de) | 2005-10-27 |
Family
ID=27108923
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE69731544T Expired - Fee Related DE69731544T2 (de) | 1996-09-13 | 1997-09-11 | Trizyklische antitumor verbindungen mit farnesyl protein transferase inhibierender wirkung |
Country Status (12)
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6228865B1 (en) | 1997-06-17 | 2001-05-08 | Schering Corporation | Compounds useful for inhibition of farnesyl protein transferase |
| AU7815198A (en) * | 1997-06-17 | 1999-01-04 | Schering Corporation | Compounds useful for inhibition of farnesyl protein transferase |
| US5852034A (en) * | 1997-06-17 | 1998-12-22 | Schering Corporation | Benzo(5,6)cycloheptapyridine cyclic ureas and lactams useful as farnesyl protein transferase inhibitors |
| US5925639A (en) * | 1997-06-17 | 1999-07-20 | Schering Corporation | Keto amide derivatives useful as farnesyl protein transferase inhibitors |
| US6218401B1 (en) | 1997-06-17 | 2001-04-17 | Schering Corporation | Phenyl-substituted tricyclic inhibitors of farnesyl-protein transferase |
| JP2002504142A (ja) * | 1997-06-17 | 2002-02-05 | シェーリング コーポレイション | ファルネシルタンパク質トランスフェラーゼの阻害に有用なベンゾ（５，６）シクロヘプタ（１，２−ｂ）ピリジン誘導体 |
| US6211193B1 (en) | 1997-06-17 | 2001-04-03 | Schering Corporation | Compounds useful for inhibition of farnesyl protein transferase |
| EP1047675A1 (en) | 1998-01-21 | 2000-11-02 | Millennium Pharmaceuticals, Inc. | Chemokine receptor antagonists and methods of use therefor |
| IL137266A0 (en) | 1998-01-21 | 2001-07-24 | Millennium Pharm Inc | Heterocyclic chemokine receptor antagonists and pharmaceutical compositions containing the same |
| US6613905B1 (en) | 1998-01-21 | 2003-09-02 | Millennium Pharmaceuticals, Inc. | Chemokine receptor antagonists and methods of use therefor |
| US6509346B2 (en) | 1998-01-21 | 2003-01-21 | Millennium Pharmaceuticals, Inc. | Chemokine receptor antagonists and methods of use therefor |
| ATE274498T1 (de) * | 1998-07-24 | 2004-09-15 | Russinsky Ltd | Verfahren zur herstellung von benzocycloheptapyridin-11-one |
| US7271176B2 (en) | 1998-09-04 | 2007-09-18 | Millennium Pharmaceuticals, Inc. | Chemokine receptor antagonists and methods of use thereof |
| US6503926B2 (en) | 1998-09-04 | 2003-01-07 | Millennium Pharmaceuticals, Inc. | Chemokine receptor antagonists and methods of use therefor |
| US6288083B1 (en) | 1998-09-04 | 2001-09-11 | Millennium Pharmaceuticals, Inc. | Chemokine receptor antagonists and methods of use therefor |
| US6262216B1 (en) | 1998-10-13 | 2001-07-17 | Affymetrix, Inc. | Functionalized silicon compounds and methods for their synthesis and use |
| US6638950B2 (en) | 2000-06-21 | 2003-10-28 | Bristol-Myers Squibb Pharma Company | Piperidine amides as modulators of chemokine receptor activity |
| US7342016B2 (en) | 2000-08-30 | 2008-03-11 | Schering Corporation | Farnesyl protein transferase inhibitors as antitumor agents |
| US7541365B2 (en) | 2001-11-21 | 2009-06-02 | Millennium Pharmaceuticals, Inc. | Chemokine receptor antagonists and methods of use therefor |
| DE60314535T2 (de) * | 2002-10-03 | 2008-02-21 | Schering Corp. | Enantioselective alkylierung von trizyklischen verbindungen |
| TWI291467B (en) | 2002-11-13 | 2007-12-21 | Millennium Pharm Inc | CCR1 antagonists and methods of use therefor |
| JP4614770B2 (ja) * | 2002-11-18 | 2011-01-19 | シェーリング コーポレイション | アンドロゲン依存性疾患を処置するための１７β−ヒドロキシステロイドデヒドロゲナーゼタイプ３インヒビター |
| US7417026B2 (en) | 2003-08-13 | 2008-08-26 | Children's Hospital Medical Center | Mobilization of hematopoietic cells |
| WO2005058823A1 (ja) * | 2003-12-17 | 2005-06-30 | Takeda Pharmaceutical Company Limited | ウレア誘導体、その製造法及び用途 |
| CA2559282A1 (en) * | 2004-03-18 | 2005-09-29 | Brigham And Women's Hospital, Inc. | Methods for the treatment of synucleinopathies |
| CN113549072B (zh) * | 2020-04-23 | 2024-12-06 | 鲁南制药集团股份有限公司 | 一种托法替布杂质ⅰ的制备方法 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5089496A (en) * | 1986-10-31 | 1992-02-18 | Schering Corporation | Benzo[5,6]cycloheptapyridine compounds, compositions and method of treating allergies |
| US4826853A (en) * | 1986-10-31 | 1989-05-02 | Schering Corporation | 6,11-Dihydro-11-(N-substituted-4-piperidylidene)-5H-benzo(5,6)cyclohepta(1,2-B)pyridines and compositions and methods of use |
| KR920014799A (ko) * | 1991-01-18 | 1992-08-25 | 나오가따 다이도 | 신규벤조[5,6]시클로헵타[1,2-b]피리딘 유도체 및 이를 함유하는 항알레르기제 |
| US5721236A (en) * | 1993-10-15 | 1998-02-24 | Schering Corporation | Tricyclic carbamate compounds useful for inhibition of G-protein function and for treatment of proliferative diseases |
| ZA947970B (en) * | 1993-10-15 | 1996-07-12 | Schering Corp | Tricyclic carbamate compounds useful for inhibition of g-protein function and for treatment of proliferative diseases |
| US5719148A (en) * | 1993-10-15 | 1998-02-17 | Schering Corporation | Tricyclic amide and urea compounds useful for inhibition of g-protein function and for treatment of proliferative diseases |
| IL111235A (en) * | 1993-10-15 | 2001-03-19 | Schering Plough Corp | Medicinal preparations for inhibiting protein G activity and for the treatment of malignant diseases, containing tricyclic compounds, some such new compounds and a process for the preparation of some of them |
| US5700806A (en) * | 1995-03-24 | 1997-12-23 | Schering Corporation | Tricyclic amide and urea compounds useful for inhibition of G-protein function and for treatment of proliferative diseases |
| IL117798A (en) * | 1995-04-07 | 2001-11-25 | Schering Plough Corp | Tricyclic compounds useful for inhibiting the function of protein - G and for the treatment of malignant diseases, and pharmaceutical preparations containing them |
| US5712280A (en) * | 1995-04-07 | 1998-01-27 | Schering Corporation | Tricyclic compounds useful for inhibition of G-protein function and for treatment of proliferative diseases |
| ATE309238T1 (de) * | 1995-12-22 | 2005-11-15 | Schering Corp | Zur hemming der g-protein-funktion und zur behandlung proliferativer krankheiten geeignete tricyclische amide |
-
1997
- 1997-09-11 KR KR1019997002134A patent/KR20000036111A/ko not_active Withdrawn
- 1997-09-11 CN CN97199602A patent/CN1238770A/zh active Pending
- 1997-09-11 EP EP97910710A patent/EP0929544B1/en not_active Expired - Lifetime
- 1997-09-11 JP JP51375898A patent/JP2001521489A/ja not_active Ceased
- 1997-09-11 AU AU48011/97A patent/AU4801197A/en not_active Abandoned
- 1997-09-11 ES ES97910710T patent/ES2229340T3/es not_active Expired - Lifetime
- 1997-09-11 WO PCT/US1997/015899 patent/WO1998011092A1/en active IP Right Grant
- 1997-09-11 HU HU0001109A patent/HUP0001109A2/hu unknown
- 1997-09-11 AT AT97910710T patent/ATE282036T1/de not_active IP Right Cessation
- 1997-09-11 CA CA002266015A patent/CA2266015C/en not_active Expired - Fee Related
- 1997-09-11 DE DE69731544T patent/DE69731544T2/de not_active Expired - Fee Related
- 1997-09-11 IL IL12893197A patent/IL128931A0/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2001521489A (ja) | 2001-11-06 |
| CA2266015A1 (en) | 1998-03-19 |
| CA2266015C (en) | 2003-12-30 |
| EP0929544A1 (en) | 1999-07-21 |
| HUP0001109A2 (hu) | 2001-04-28 |
| AU4801197A (en) | 1998-04-02 |
| CN1238770A (zh) | 1999-12-15 |
| ATE282036T1 (de) | 2004-11-15 |
| DE69731544D1 (de) | 2004-12-16 |
| EP0929544B1 (en) | 2004-11-10 |
| ES2229340T3 (es) | 2005-04-16 |
| WO1998011092A1 (en) | 1998-03-19 |
| KR20000036111A (ko) | 2000-06-26 |
| IL128931A0 (en) | 2000-02-17 |
| HK1018446A1 (en) | 1999-12-24 |
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Legal Events
| Date | Code | Title | Description |
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| 8364 | No opposition during term of opposition | ||
| 8339 | Ceased/non-payment of the annual fee |